home Audience 1 Egilok s is an effective remedy for normalizing blood pressure and heart rate. Comparative analysis of Betaloc ZOK or Egiloc preparations: which is better and how they differ from each other

Egilok s is an effective remedy for normalizing blood pressure and heart rate. Comparative analysis of Betaloc ZOK or Egiloc preparations: which is better and how they differ from each other

Selective blocker of β-adrenergic receptors, has antianginal, antihypertensive and antiarrhythmic effects, reduces the automatism of the sinus node, inhibits AV conduction, reduces myocardial inotropic function and heart rate. The antihypertensive effect stabilizes at the end of the 2nd week of the drug. Reduces the number of angina attacks, reduces myocardial oxygen demand, increases exercise tolerance. In myocardial infarction, it limits the zone of ischemia of the heart muscle and prevents heart rhythm disturbance. The main advantage of the drug Egilok Retard (prolonged-release tablets) is the prolonged release of metoprolol. Therapeutic effect noted at a significantly lower concentration of metoprolol in the blood than when taking metoprolol in conventional tablet forms. Therefore, it is enough to prescribe 1 tablet per day of Egilok Retard to achieve a clinical effect.
The drug is rapidly and completely absorbed from the gastrointestinal tract (95% of the dose). The absorption of metoprolol in the retard form is significantly prolonged, which leads to a uniform concentration of the drug Egilok Retard in the blood plasma and a relative bioavailability of 80% compared with the graph of the change in the content of the drug in the blood after the administration of immediate release metoprolol. Maximum concentration in blood plasma is reached 1.5 hours after oral intake and after 2-6 hours - the drug in the form of a retard. Plasma protein binding - 12%. The volume of distribution is 5.6 l/kg of body weight. Metoprolol is metabolized in the liver, its metabolites do not show activity. About 5% of the dose is excreted unchanged in the urine.

Indications for use of the drug Egilok

AG (arterial hypertension);
CAD: stable or unstable angina(with the exception of Prinzmetal's angina);
heart failure;
heart rhythm disorders (sinus, supraventricular tachycardia; ventricular extrasystole);
arrhythmia against the background of mitral valve prolapse;
secondary prevention after myocardial infarction;
functional disorders I cardiac activity, accompanied by tachycardia;
hyperthyroidism;
prevention of migraine attacks.

The use of the drug Egilok

With hypertension (arterial hypertension), the initial dose of Egilok Retard is 50 mg / day in 1 dose. The daily dose can be gradually increased to 100-200 mg in 1 dose. Egilok Retard can be used with other antihypertensive drugs to increase the hypotensive effect.
For the treatment of angina pectoris, the dose is 50 mg 1 time per day, with further dose titration to the clinically optimal. If necessary, the dose can be increased to 100-200 mg in 1 dose. Egilok Retard can be used with other antianginal drugs.
In heart failure, the initial dose is 25 mg / day. If necessary, every 2 weeks the dose can be increased to 50 mg, after another 2 weeks - up to 100 mg, if necessary, after 2 weeks to 200 mg.
With arrhythmia, the initial dose is 50-200 mg / day in 1 dose.
After myocardial infarction, for the purpose of its secondary prevention, the dose is selected individually under the control of heart rate and blood pressure.
For the prevention of migraine attacks, the usual dose is 100-200 mg / day in 1 dose. Tablets are taken 1 time per day (in the morning), without chewing and drinking plenty of liquid.
The drug can also be taken with food or on an empty stomach.

Contraindications to the use of the drug Egilok

G hypersensitivity to metoprolol or other components of the drug; AV block II-III degree, severe sinus bradycardia(heart rate ≤50 bpm), arterial hypotension, acute decompensated heart failure, severe peripheral circulation disorders; cardiogenic shock, severe disorders of peripheral circulation, BA, sick sinus syndrome.

Side effects of the drug Egilok

Decreased heart rate, blood pressure. There may also be a violation of AV conduction, symptoms of heart failure, depression. There may be such side effects like fatigue, headache, dizziness, sleep disturbance. In many cases, these phenomena are temporary and disappear on their own with a decrease in the dose of the drug.
Rarely, nonspecific skin reactions and cold extremities, vomiting, diarrhea, constipation, bronchospasm, thrombocytopenia, and liver dysfunction occur.
If you experience any other side effects that are not listed in the instructions, you must inform your doctor.

Special instructions for the use of the drug Egilok

With caution, the drug should be used in the treatment of patients with diabetes mellitus, with peripheral arterial disease, pheochromocytoma (Egilok Retard may be used only in combination with α-adrenergic receptor blockers), impaired renal and hepatic function. Before starting treatment, it is necessary to determine the function of the liver and kidneys. End therapy with Egilok Retard should be gradual. Sudden termination treatment, especially when cardiovascular pathology, may lead to deterioration of the condition (withdrawal syndrome).
The use of Egilok Retard may cause fatigue or slight dizziness. Therefore, during the treatment period, it is necessary to refrain from managing vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
If the patient seeks medical help or needs to be surgical treatment it is necessary to warn the doctor about the patient taking the drug Egilok Retard.
The appointment of the drug Egilok Retard during pregnancy and lactation is possible if the potential benefit to the mother outweighs the risk to the child.

Interactions of the drug Egilok

Caution is necessary when using the drug simultaneously with:

verapamil and diltiazem - the risk of hypotension, bradycardia, atrioventricular blockade, asystole;
clonidine - taking clonidine must be completed a few days after the end of metoprolol in order to avoid the development of a withdrawal syndrome;
narcotic drugs - the risk of developing a cardiodepressive effect;
ergotamine - increases the vasoconstrictor effect);
some drugs that affect the central nervous system: sleeping pills - bromazepam, lorazepam;
tranquilizers - chlordiazepoxide, trimetacin, tofisopam;
tri- and tetracyclic antidepressants - citalopram, moclobemide;
neuroleptics - chlorpromazine, triflupromazine - and alcohol - risk arterial hypotension, influence on the central nervous system;
NSAIDs, such as indomethacin - it is possible to reduce the antihypertensive effect of metoprolol;
estrogen, such as norethindrone, norgestrel - the antihypertensive effect of metoprolol is reduced;
hypoglycemic by oral means, for example, chlorpropamide, glibenclamide, tolbutamide and insulin - enhancing their hypoglycemic effect, masking the symptoms of hypoglycemia;
curare-like muscle relaxants - increased neuromuscular blockade;
H2 receptor antagonists, such as cimetidine - it is possible to increase the bioavailability of the drug);
rifampicin, barbiturates, such as phenobarbital, secobarbital, pentobarbital - it is possible to reduce the antihypertensive effect of metoprolol.

Particular caution is required when used with ganglion-blocking drugs and other β-adrenergic blockers, sympathomimetics, class I antiarrhythmic drugs.

Overdose of the drug Egilok, symptoms and treatment

Symptoms: arterial hypotension, sinus bradycardia, AV blockade, heart failure, cardiogenic shock, asystole, nausea, vomiting, cyanosis, bronchospasm, loss of consciousness, coma.
Treatment: gastric lavage, activated carbon, with severe hypotension - β-adrenergic agonists (norepinephrine) or intravenous atropine (with bradycardia). If there is no effect, dopamine, dobutamine should be prescribed. Glucagon (1-10 mg) may be effective. IN severe cases implantation of an artificial pacemaker may be necessary. Bronchospasm is eliminated by the introduction of intravenous β2-adrenergic agonists. Metoprolol is practically not excreted from the body by hemodialysis.

Storage conditions of the drug Egilok

At a temperature of 15-25 °C.

List of pharmacies where you can buy Egilok:

Saint Petersburg

Egilok is a remedy for
treatment of diseases of the cardiovascular system.

pharmachologic effect

Egilok, according to the instructions, refers to beta1-adrenergic blocking agents.

Main active substance- metoprolol. It has antianginal, antiarrhythmic, pressure-lowering effects. By blocking beta1-adrenergic receptors, Egilok reduces the excitatory effect of the sympathetic nervous system on the heart muscle, quickly reduces heart rate and blood pressure. The hypotensive effect of the drug is long-lasting, as peripheral vascular resistance decreases gradually.

On the background long-term use Egilok with high blood pressure significantly reduces the mass of the left ventricle, it relaxes better in the diastolic phase. According to reviews, Egilok is able to reduce mortality from cardiovascular pathology in males with a moderate increase in pressure.

Like analogues, Egilok reduces the heart's need for oxygen due to a decrease in pressure and heart rate. Due to this, diastole is lengthened - the time during which the heart rests, which improves its blood supply and the absorption of oxygen from the blood. This action reduces the frequency of angina attacks, and against the background of asymptomatic episodes of ischemia physical state and the patient's quality of life is greatly improved.

The use of Egilok reduces the frequency of ventricular heart contractions in atrial fibrillation, ventricular premature beats and supraventricular tachycardia.

Compared with non-selective beta-blockers of Egilok's analogues, it has less pronounced vasoconstrictor and bronchial properties, and it also has less effect on carbohydrate metabolism.

Against the background of taking the drug for several years, blood cholesterol is significantly reduced.

Release form Egilok

Egilok is produced in tablets of 25, 50 and 100 mg.

Indications for Egilok

The drug is used to treat angina pectoris, myocardial infarction, arterial hypertension, including in elderly patients, rhythm disturbances, complex treatment migraine.

Contraindications

According to the instructions, Egilok can not be used in case of atrioventricular blockade of 2 and 3 degrees, weaknesses sinus node, depressions blood pressure below 90-100 mm Hg. Art., with sinus bradycardia with a heart rate below 50-60 beats per minute.

Hypersensitivity to the components of the drug is also a contraindication.

Instructions for use Egilok

The drug in tablets is taken regardless of food, dose selection is strictly individual and should be carried out gradually. More than 200 mg / day Egilok can not be taken. To achieve the effect, regular intake of the drug is important.

To reduce blood pressure start with a dose of 25-50 mg 2 times a day (morning, evening), if necessary, increasing the dose.

For the treatment of angina pectoris
take 25-50 mg 2-3 times a day, if the effect is insufficient, the dose is increased to 200 mg / day or another drug is added to the treatment regimen. It is advisable to maintain a heart rate of 55-60 beats / min at rest and no more than 110 beats / min during exercise while taking the medication.

As maintenance therapy after myocardial infarction, 100-200 mg / day is prescribed in 2 divided doses.

With cardiac arrhythmias, the initial dose is 25-50 mg 2-3 times a day, in case of insufficient effectiveness, increase it to 200 mg / day or add another antiarrhythmic agent to the treatment regimen.

If there are indications for Egilok in the treatment of migraine attacks, its dose in this case is 100 mg / day in 2 divided doses.

At concomitant pathology kidney and liver, as well as in elderly patients, dose adjustment of Egilok is not required.

When a patient uses contact lenses, the patient should be aware of possible appearance discomfort due to a decrease in the production of tear fluid during treatment with this agent.

If planned surgery against the background of taking Egilok, it is necessary to warn the anesthetist about this so that he can choose adequate means for anesthesia with a minimal inotropic effect. It is not required to cancel the drug.

It is necessary to complete the treatment with the drug gradually, reducing the dose every 2 weeks. Abrupt withdrawal of the drug may worsen the patient's condition.

Side effects

According to reviews, Egilok is sometimes able to cause headache, fatigue, depression, insomnia, dizziness, decreased concentration, decreased heart rate, shortness of breath, bronchospasm, rhinitis, nausea, diarrhea, vomiting, abdominal pain, increased sweating, allergic reactions.

Sincerely,

International name

Metoprolol (Metoprolol)

Group affiliation

Selective beta1-blocker

Dosage form

Tablets, long-acting tablets, long-acting enteric coated tablets, long-acting tablets

pharmachologic effect

Cardioselective beta1-blocker. It does not have a membrane-stabilizing effect and does not have an internal CMA. It has hypotensive, antiangial and antiarrhythmic effects.

Blocking in not high doses beta1-adrenergic receptors of the heart, reduces the formation of cAMP from ATP stimulated by catecholamines, reduces intracellular Ca2+ current, has a negative chrono-, dromo-, batmo- and inotropic effect (slows heart rate, inhibits conductivity and excitability, reduces myocardial contractility).

OPSS at the beginning of the use of beta-blockers (in the first 24 hours after oral administration) increases (as a result of a reciprocal increase in the activity of alpha-adrenergic receptors and the elimination of stimulation of beta2-adrenergic receptors), which after 1-3 days returns to the original, and decreases with long-term administration.

The hypotensive effect is due to a decrease in the IOC and renin synthesis, inhibition of the activity of the renin-angiotensin system (has greater value in patients with initial hypersecretion of renin) and the central nervous system, restoration of the sensitivity of baroreceptors of the aortic arch (there is no increase in their activity in response to a decrease in blood pressure) and, as a result, a decrease in peripheral sympathetic influences. Reduces high blood pressure at rest, during physical exertion and stress. The hypotensive effect develops quickly (systolic blood pressure decreases after 15 minutes, maximum - after 2 hours) and lasts for 6 hours, diastolic blood pressure changes more slowly: a stable decrease is observed after several weeks of regular intake.

The antianginal effect is determined by a decrease in myocardial oxygen demand as a result of a decrease in heart rate (lengthening of diastole and improvement in myocardial perfusion) and contractility, as well as a decrease in myocardial sensitivity to the effects of sympathetic innervation. Reduces the number and severity of angina attacks and improves tolerability physical activity. By increasing LV end-diastolic pressure and increasing stretch muscle fibers ventricular function may increase oxygen demand, especially in patients with CHF.

The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity sympathetic nervous system, increased levels of cAMP, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and a slowdown in AV conduction (mainly in the antegrade and, to a lesser extent, in the retrograde directions through the AV node) and along additional pathways.

With supraventricular tachycardia, atrial fibrillation, sinus tachycardia with functional diseases heart and thyrotoxicosis slows the heart rate or may even lead to the restoration of sinus rhythm.

Prevents the development of migraine.

Unlike non-selective beta-blockers, when administered in medium therapeutic doses ax has a less pronounced effect on organs containing beta2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism; the severity of the atherogenic action does not differ from the action of propranolol. With long-term use, it reduces the concentration of cholesterol in the blood. When used in large doses(more than 100 mg / day) has a blocking effect on both subtypes of beta-adrenergic receptors.

With intravenous infusion of metoprolol tartrate for 10 minutes or more, the maximum effect develops after 20 minutes, a decrease heart rate at doses of 5 and 10 mg is 10 and 15%, respectively.

Indications

IHD, exertional angina, unstable angina, myocardial infarction ( acute phase as well as secondary prevention).

Arterial hypertension, hypertensive crisis.

CHF (compensated) in combination with diuretics, ACE inhibitors and cardiac glycosides.

Rhythm disturbances (including with general anesthesia) - sinus tachycardia, ventricular and supraventricular arrhythmias (including supraventricular tachycardia, atrial fibrillation, atrial flutter, atrial tachycardia, tachyarrhythmias caused by digitalis, catecholamines, ventricular extrasystoles, arrhythmias against the background of prolapse of the congenital mitral valve), congenital mitral valve syndrome .

thyrotoxicosis ( complex therapy), withdrawal syndrome, migraine (prevention), tremor (essential, senile), anxiety ( ancillary treatment), akathisia on the background of neuroleptics.

Contraindications

Hypersensitivity, cardiogenic shock, AV block II-III stage, SA block, SSSU, sinus bradycardia (HR less than 50/min), acute HF or decompensated CHF, Prinzmetal's angina, arterial hypotension, acute myocardial infarction (P-Q more than 0.24 s or systolic BP less than 100 mm Hg); lactation period, concomitant use of MAO inhibitors or simultaneous intravenous administration of verapamil. C with caution. Diabetes, metabolic acidosis, bronchial asthma, COPD (emphysema, chronic obstructive bronchitis), liver failure, chronic renal failure, myasthenia gravis, pheochromocytoma, thyrotoxicosis, depression (including history), psoriasis, obliterating diseases of peripheral vessels ("intermittent" claudication, Raynaud's syndrome), pregnancy, childhood(effectiveness and safety not determined), elderly age.

Side effects

From the nervous system: fatigue, weakness, headache, slowing down the speed of mental and motor reactions. Rare: paresthesias in the extremities (in patients with "intermittent" claudication and Raynaud's syndrome), tremor, convulsions, depression, anxiety, decreased attention, drowsiness, insomnia, "nightmares" dreams, confusion or short-term memory loss, hallucinations, asthenia, myasthenia gravis .

From the sensory organs: rarely - decreased vision, decreased secretion of lacrimal fluid, dryness and soreness of the eyes, conjunctivitis, tinnitus, hearing loss.

From the CCC: sinus bradycardia, decreased blood pressure, orthostatic hypotension (dizziness, sometimes loss of consciousness). Rarely - a decrease in myocardial contractility, development (aggravation) of CHF (edema, swelling of the feet and / or lower legs, shortness of breath), cardiac arrhythmias, angiospasm manifestation (increased peripheral circulatory disorders, cooling lower extremities, Raynaud's syndrome), myocardial conduction disturbance, cardialgia. Very rarely - aggravation of pre-existing AV conduction disorders.

From the side digestive system: nausea, vomiting, abdominal pain, dry mouth, constipation or diarrhea, in some cases - abnormal liver function ( dark urine, yellowness of the sclera or skin, cholestasis), changes in taste.

From the side skin: skin rash (exacerbation of psoriasis), psoriasis-like skin reactions, skin flushing, exanthema, photodermatosis, increased sweating, reversible alopecia.

From the side respiratory system: nasal congestion, bronchospasm when administered in high doses (loss of selectivity and / or in predisposed patients), shortness of breath.

From the side endocrine system: hyperglycemia (in patients with non-insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroid state.

Allergic reactions: urticaria, pruritus, rash.

Laboratory indicators: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased activity of "liver" enzymes, hyperbilirubinemia.

Effect on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia.

Other: pain in the back or joints, weight gain, decreased libido and / or potency, with a sharp cessation of treatment - "withdrawal" syndrome (increased angina attacks, increased blood pressure).

Application and dosage

Inside, with a meal or immediately after a meal, the tablets can be divided in half, but not chewed and washed down with liquid, for prolonged-release dosage forms - swallow whole, do not crush, do not break (except for metoprolol succinate and tartrate), do not chew.

With arterial hypertension average dose- 100-150 mg / day in 1-2 doses, if necessary - 200 mg / day.

With angina - 50 mg 2-3 times a day.

With hyperkinetic cardiac syndrome (including thyrotoxicosis) - 50 mg 1-2 times a day.

With tachyarrhythmia - 50 mg 2-3 times a day, if necessary - 200-300 mg / day.

Secondary prevention of myocardial infarction - 200 mg / day.

Prevention of migraine - 100-200 mg / day in 2-4 doses.

For the relief of paroxysmal supraventricular tachycardia, it is administered parenterally, in a hospital setting. Enter slowly, a dose of 2-5 mg (1-2 mg / min). If there is no effect, the administration can be repeated after 5 minutes. Increasing the dose above 15 mg usually does not lead to a greater severity of action. After stopping the attack of arrhythmia, patients are transferred to oral administration at a dose of 50 mg 4 times a day, with the first dose being taken 15 minutes after the cessation of intravenous administration.

IN acute stage myocardial infarction, immediately after hospitalization of the patient (with constant monitoring of hemodynamics: ECG, heart rate, AV conduction, blood pressure), a bolus of 5 mg should be administered intravenously, repeated every 2 minutes until a total dose of 15 mg is reached. With good tolerance after 15 minutes - inside, 25-50 mg every 6 hours, for 2 days. In patients who have not tolerated the full intravenous dose, oral administration should be initiated starting with half the dose. Maintenance therapy continues at doses of 200 mg / day (for 2 doses), for 3 months-3 years.

Renal failure does not require dose adjustment. At liver failure it is advisable to prescribe other beta-blockers that are not metabolized in the liver.

special instructions

Monitoring of patients taking beta-blockers includes monitoring heart rate and blood pressure (at the beginning of admission - daily, then 1 time in 3-4 months), blood glucose concentration in diabetic patients (1 time in 4-5 months). The patient should be taught how to calculate heart rate and instruct about the need for a medical consultation if the heart rate is less than 50/min.

It is possible to increase the severity of allergic reactions (against the background of a burdened allergic history) and the lack of effect from the introduction usual doses epinephrine.

In elderly patients, it is recommended to monitor kidney function (1 time in 4-5 months). May exacerbate symptoms of peripheral arterial circulation. Patients with cardiac arrhythmias, whose systolic blood pressure is below 100 mm Hg, should be administered intravenously only if special measures precautions (there is a risk of a further decrease in blood pressure). Cancellation of the drug is carried out gradually, reducing the dose within 10 days.

With arterial hypertension, the effect occurs after 2-5 days, a stable effect is noted after 1-2 months.

With angina pectoris, the selected dose of the drug should provide heart rate at rest in the range of 55-60 beats / min, with exercise - no more than 110 beats / min. In "smokers" the effectiveness of beta-blockers is lower.

At combination therapy with clonidine, the latter should be discontinued a few days after the abolition of metoprolol, in order to avoid hypertensive crisis. At a dose above 200 mg / day, cardioselectivity decreases.

Metoprolol may mask some clinical manifestations thyrotoxicosis (eg tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, as it can exacerbate symptoms.

In diabetes, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentration to normal level.

If necessary, prescribing to patients with bronchial asthma beta2-agonists are used as concomitant therapy; with pheochromocytoma - alpha-blockers.

If it is necessary to carry out surgical intervention it is necessary to warn the anesthesiologist about the ongoing therapy (the choice of drugs for general anesthesia with a minimal negative inotropic effect), drug withdrawal is not recommended.

Reciprocal activation of n.vagus can be eliminated by intravenous atropine (1-2 mg).

Drugs that reduce catecholamine reserves (for example, reserpine) can enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect an excessive decrease in blood pressure or bradycardia.

In the case of the appearance in elderly patients of increasing bradycardia (less than 50 / min), arterial hypotension (systolic blood pressure below 100 mm Hg), AV blockade, bronchospasm, ventricular arrhythmias, severe impairment of liver and kidney function, it is necessary to reduce the dose or stop treatment. It is recommended to stop therapy with the appearance of skin rashes and the development of depression caused by taking beta-blockers.

Cancellation of the drug is carried out gradually, reducing the dose within 10 days. With a sharp cessation of treatment, a "withdrawal" syndrome may occur (increased angina attacks, increased blood pressure). Particular attention should be paid to patients with angina pectoris when discontinuing the drug.

Patients using contact lenses, should take into account that against the background of treatment with beta-blockers, a decrease in the production of lacrimal fluid is possible.

During pregnancy, it is prescribed only for strict indications (due to possible development neonatal bradycardia, hypotension, hypoglycemia, and respiratory paralysis). Treatment must be interrupted 48-72 hours before delivery. In cases where this is not possible, it is necessary to ensure strict monitoring of newborns within 48-72 hours after delivery.

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

Interaction

Allergens used for immunotherapy or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving metoprolol. Iodine-containing radiopaque drugs for intravenous administration increase the risk of developing anaphylactic reactions.

Phenytoin when administered intravenously, drugs for inhalation general anesthesia (hydrocarbon derivatives) increase the severity of the cardiodepressive effect and the likelihood of lowering blood pressure.

Changes the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure).

Reduces the clearance of lidocaine and xanthines (except diphylline) and increases their plasma concentration, especially in patients with initially increased clearance of theophylline under the influence of smoking.

The hypotensive effect is weakened by NSAIDs (Na + retention and blockade of Pg synthesis by the kidneys), GCS and estrogens (Na + retention).

Cardiac glycosides, methyldopa, reserpine and guanfacine, BMCC (verapamil, diltiazem), amiodarone and other antiarrhythmic drugs increase the risk of developing or worsening bradycardia, AV blockade, cardiac arrest and heart failure. Nifedipine can lead to a significant decrease in blood pressure.

Diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs can lead to an excessive decrease in blood pressure.

Prolongs the action of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins.

Tri- and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedative and hypnotic drugs increase CNS depression.

Simultaneous use with MAO inhibitors is not recommended due to a significant increase in the hypotensive effect, a break in treatment between taking MAO inhibitors and metoprolol should be at least 14 days.

Non-hydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders.

Reviews about the drug Egilok: 1

I take egilok 1, 2 tons in the morning - there is dizziness (50 mg)

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Do you use Egilok as an analogue or vice versa?

Virtually all drugs and alcoholic beverages are mutually exclusive of taking each other at the same time. Egilok and alcohol are no exception.

Feedback from both doctors and patients that form medical statistics on this issue, confirm the strong recommendation to avoid such a combination.

Egilok is prescribed for the treatment of the heart and blood vessels. The medicine has the following actions:

stops attacks of stenocardia, and also warns them;
restores all types of cardiac arrhythmias, such as extrasystole, atrial fibrillation, paroxysmal tachycardia, ventricular fibrillation;
localizes migraine attacks;

The drug is indicated for the rehabilitation of patients who have had a heart attack. In addition, it lowers blood pressure and has a long therapeutic effect. Contraindications to taking medication, side effects and special conditions required for successful therapy are described in detail in the annotation to the drug.

The effect of alcohol on the cardiovascular system

Each intake of alcohol makes all body systems work in an enhanced mode. Acting through the blood, alcohol speeds up the heartbeat, increases blood flow, sharply expands and constricts blood vessels. Ultimately, this becomes the cause of their destruction.

On the heart system, alcohol abuse affects the following:

slows down the work of the heart;
leads to deformation heart valve, and as a consequence, its rupture;
provokes frequent failures in the functions of the parts of the nervous system, including the area that regulates the operator level of all body systems;
forms blood clots
generates changes in the work of the myocardium.

Systematic damage in the system of the heart and blood vessels, which occurs under the influence of strong drinks, becomes the basis for the development of diseases: cardiomyopathy, coronary disease, atherosclerosis, heart attack, stroke.

Beer in large doses leads to: an increase in heart volume, frequent heartbeat sustained high blood pressure.

Unhealthy functioning of the entire cardiovascular system poses an extreme danger to human health and often leads to disability or lethal outcome even in young people.

Combining Egilok and alcohol: dangerous consequences

It is impossible to take Egilok and alcohol at the same time, in a categorical form. This will cause complications, the consequences of which can adversely affect human health in general, death is not excluded.

Opposite action

First, the effect that medicine and alcoholic beverages have is diametrically opposed. Therefore, their simultaneous use can cause sudden cardiovascular failure. Its outcome may be death. In medicine, this phenomenon is called collapse. It is characterized by a sudden drop in blood pressure, typical features which are exhaustion and severe dizziness. Often the patient loses consciousness. The collapse calls for immediate medical care. Delay threatens a person with death.

Overdose

Secondly, an overdose of ethanol is a fairly common occurrence when trying to combine Egilok with alcohol. For the process of breaking down ethyl alcohol in the body, adrenaline is required. This biological substance actively influences the rate of ethanol oxidation. As a result, alcohol breaks down faster and is excreted naturally, without lingering in internal organs and blood. Metoprolol, the main component of Egilok, counteracts adrenaline by blocking its work. This causes a slow oxidation of alcohol. As a result, there is an accumulation of ethanol, which leads to an overdose.

First of all, the central nervous system will suffer, which will be reflected in the deterioration general condition health: inhibited speech, lack of vigor and mobility, difficulty in determining one's location. As intoxication worsens, additional signs of complications appear: difficulty breathing, a drop in blood pressure, impaired consciousness. The patient may fall into a coma or die if medical assistance is not provided.

Consequences for the liver

Thirdly, the effect on the liver. This is another reason to avoid combining Egilok and alcohol. Taking the medicine significantly affects the functioning of the gland. Alcohol not only enhances this load, but also poisons the liver with toxic substances. Therefore, there is a double Negative influence on an organ that accelerates the formation of diseases, for example, toxic hepatitis. All liver diseases are initial stages without obvious symptoms. This increases the risk of missing the development of an anomaly and seriously threatens human health.

For reference: Toxic hepatitis- liver disease, formed under the influence of various harmful substances, including chemicals: drugs; alcohol; poisons contained in plants and so on.

Each drug is accompanied by instructions for use, where the manufacturer indicates compatible this remedy with alcohol or not. In fairness, it should be said that therapy with the use of certain medications allows, episodically, the intake of a small amount of wine. Egilok is not one of them.

Registration number: P No. 015639/01 03/17/2009

Trade name: Egilok ®

International non-proprietary name: metoprolol

PHARMACOLOGICAL PROPERTIES

Mechanism of action:

Metoprolol inhibits the effect of increased activity sympathetic system on the heart, and also causes a rapid decrease in heart rate, contractility, cardiac output and blood pressure.

At arterial hypertension metoprolol lowers blood pressure in patients in the standing and lying position. The long-term antihypertensive effect of the drug is associated with a gradual decrease in total peripheral vascular resistance. In arterial hypertension, long-term use of the drug leads to a statistically significant decrease in the mass of the left ventricle and an improvement in its diastolic function. In men with mild to moderate hypertension, metoprolol reduces mortality from cardiovascular causes (primarily sudden death, fatal and non-fatal heart attack and stroke).

Like other beta-blockers, metoprolol reduces myocardial oxygen demand by reducing systemic arterial pressure, heart rate and myocardial contractility. The decrease in heart rate and the corresponding lengthening of diastole when taking metoprolol provide improved blood supply and oxygen uptake by the myocardium with impaired blood flow. Therefore, in angina pectoris, the drug reduces the number, duration and severity of attacks, as well as asymptomatic manifestations of ischemia, and improves physical performance patient. In myocardial infarction, metoprolol reduces the mortality rate by reducing the risk sudden death. This effect is primarily associated with the prevention of episodes of ventricular fibrillation. A decrease in mortality can also be observed with the use of metoprolol in both the early and late phases of myocardial infarction, as well as in high-risk patients and patients with diabetes mellitus. The use of the drug after myocardial infarction reduces the likelihood of non-fatal re-infarction. In chronic heart failure against the background of idiopathic hypertrophic obstructive cardiomyopathy, metoprolol tartrate, taken starting from low doses (2x5 mg / day) with a gradual increase in dose, significantly improves heart function, quality of life and physical endurance of the patient.

With supraventricular tachycardia, atrial fibrillation and ventricular premature beats, metoprolol reduces the frequency of ventricular contractions and the number of ventricular extrasystoles.

At therapeutic doses, the peripheral vasoconstrictor and bronchoconstrictor effects of metoprolol are less pronounced than the same effects of non-selective beta-blockers.

Compared with non-selective beta-blockers, metoprolol has less effect on insulin production and carbohydrate metabolism. It does not increase the duration of hypoglycemic episodes.

Metoprolol causes a slight increase in the concentration of triglycerides and a slight decrease in the concentration of free fatty acids in blood serum. There is a significant decrease in the total concentration of serum cholesterol after several years of taking metoprolol.

Metoprolol is rapidly and completely absorbed from the gastrointestinal tract. The drug is characterized by linear pharmacokinetics in the therapeutic dose range. The maximum plasma concentration is reached 1.5-2 hours after ingestion. After absorption, metoprolol is largely metabolized by the primary passage through the liver. The bioavailability of metoprolol is approximately 50% with a single dose and approximately 70% with regular administration.

Reception simultaneously with food can increase the bioavailability of metoprolol by 30-40%. Metoprolol is slightly (~ 5-10%) bound to plasma proteins. The volume of distribution is 5.6 l/kg.

Metoprolol is metabolized in the liver by cytochrome P-450 isoenzymes. Metabolites do not have pharmacological activity.

Half-life (t 1/2) an average of 3.5 hours (from 1 to 9 hours). The total clearance is approximately 1 l / min.

Approximately 95% of the administered dose is excreted by the kidneys, 5% in the form of unchanged metoprolol. In some cases, this value can reach 30%.

Significant changes in the pharmacokinetics of metoprolol in elderly patients have not been identified.

Impaired renal function does not affect the systemic bioavailability or excretion of metoprolol. However, in these cases, there is a decrease in the excretion of metabolites. In severe renal failure (glomerular filtration rate less than 5 ml / min), there is a significant accumulation of metabolites. However, this accumulation of metabolites does not increase the degree of beta-adrenergic blockade.

Impaired liver function has little effect on the pharmacokinetics of metoprolol. However, in severe liver cirrhosis and after a porto-caval shunt, bioavailability may increase and total clearance from the body may decrease. After porto-caval shunting, the total clearance of the drug from the body is approximately 0.3 l / min, and the area under the concentration-time curve increases by approximately 6 times compared with that in healthy volunteers.

Arterial hypertension (in monotherapy or (if necessary) in combination with other antihypertensive drugs); functional disorders of cardiac activity, accompanied by tachycardia.

Ischemic heart disease: myocardial infarction (secondary prevention - complex therapy), prevention of angina attacks.

Heart rhythm disturbances (supraventricular tachycardia, ventricular extrasystole). Hyperthyroidism (complex therapy). Prevention of migraine attacks.

Hypersensitivity to metoprolol or any other component of the drug, as well as other beta-blockers; atrioventricular block (AV) II or III degree; sinoatrial blockade; sinus bradycardia (heart rate less than 50/min), sick sinus syndrome; cardiogenic shock; severe disorders of peripheral circulation; heart failure in the stage of decompensation, age up to 18 years (due to the lack of sufficient clinical data), simultaneous intravenous administration of verapamil, severe bronchial asthma and pheochromocytoma without the simultaneous use of alpha-blockers.

Due to the lack of clinical data, Egioloc ® is contraindicated in acute infarction myocardium, accompanied by a heart rate below 45 beats / min, with a PQ interval of more than 240 ms, and systolic blood pressure below 100 mm Hg.

Diabetes mellitus, metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease (COPD), renal / hepatic failure, myasthenia gravis, pheochromocytoma (when used simultaneously with alpha-blockers), thyrotoxicosis, AV blockade of the 1st degree, depression (including in history), psoriasis, obliterating peripheral vascular disease ("intermittent" claudication, Raynaud's syndrome), pregnancy, lactation, old age, in patients with an aggravated allergic history (a decrease in response to the use of adrenaline is possible).

USE IN PREGNANCY AND LACTATION

The use of the drug is not recommended during pregnancy. The use of the drug is possible only if the benefit to the mother outweighs the potential risk to the fetus. If the drug is necessary, you should carefully monitor the fetus, and then the newborn for several days (48 - 72 hours) after birth, as bradycardia, respiratory depression, lowering blood pressure and hypoglycemia may develop.

Despite the fact that when taking therapeutic doses of metoprolol, only small amounts of the drug are released into breast milk, the newborn should be kept under observation (possible bradycardia). The use of the drug during lactation is not recommended. If necessary, the use of the drug during lactation is recommended to stop breastfeeding.

METHOD OF APPLICATION AND DOSES

Egilok ® tablets are taken orally. Tablets can be taken with or without food. If necessary, the tablet can be broken in half. The dose should be adjusted gradually and individually to avoid excessive bradycardia. Maximum daily dose is 200 mg. Recommended doses:

Arterial hypertension

With mild or moderate degree arterial hypertension initial dose of 25-50 mg twice a day (morning and evening). If necessary, the daily dose can be gradually increased to 100-200 mg / day or another antihypertensive agent can be added.

angina pectoris

Initial dose of 25-50 mg two to three times a day. Depending on the effect, this dose can be gradually increased to 200 mg per day or another antianginal drug can be added.

Supportive care after myocardial infarction

The usual daily dose - 100 - 200 mg / day, divided into two doses (morning and evening).

Heart rhythm disorders

The initial dose is 25 to 50 mg two or three times a day. If necessary, the daily dose can be gradually increased to 200 mg / day or another antiarrhythmic agent can be added. Hyperthyroidism

The usual daily dose is 150-200 mg per day for 3-4 doses.

Functional disorders of the heart, accompanied by a sensation of palpitations The usual daily dose is 50 mg 2 times a day (morning and evening); if necessary, it can be increased to 200 mg in two divided doses.

Prevention of migraine attacks

The usual daily dose is 100 mg/day in two divided doses (morning and evening); if necessary, it can be increased to 200 mg / day in 2 divided doses.

Special patient groups

In case of impaired renal function, a change in the dosing regimen is not required.

With cirrhosis of the liver, a dose change is usually not required due to the low binding of metoprolol to plasma proteins (5-10%). In severe hepatic insufficiency (for example, after portocaval bypass surgery), it may be necessary to reduce the dose of Egilok ® .

In elderly patients, dose adjustment is not required.

Egilok ® is usually well tolerated by patients. Side effects are usually mild and reversible. The side effects listed below have been reported in clinical trials and at therapeutic application metoprolol. In some cases, the relationship of an adverse event with the use of the drug has not been reliably established. Frequency options listed below side effects defined as follows: very often: > 10%), often: 1-9.9%, infrequently: 0.1-0.9%, rarely: 0.01-0.09%, very rarely (including isolated reports) :< 0,01 %.

From the nervous system: very often - increased fatigue; often - dizziness, headache; rarely - hyperexcitability, anxiety, impotence/sexual dysfunction; infrequently - paresthesia, convulsions, depression, decreased concentration, drowsiness, insomnia, "nightmare" dreams; very rarely - amnesia / memory impairment, depression, hallucinations.

From the side of the cardiovascular system: often - bradycardia, orthostatic hypotension (in some cases, syncope is possible), coldness of the lower extremities, palpitations; infrequently - a temporary increase in symptoms of heart failure, cardiogenic shock in patients with myocardial infarction, atrioventricular block I degree; rarely - conduction disturbances, arrhythmia; very rarely - gangrene (in patients with peripheral circulatory disorders). From the digestive system: often - nausea, abdominal pain, constipation or diarrhea; infrequently - vomiting; rarely - dryness of the oral mucosa, impaired liver function.

From the side of the skin: infrequently - urticaria, increased sweating; rarely - alopecia; very rarely - photosensitivity, exacerbation of the course of psoriasis. From the respiratory system: often - shortness of breath during physical effort; infrequently - bronchospasm in patients with bronchial asthma; rarely - rhinitis.

From the sensory organs: rarely - blurred vision, dryness and / or irritation of the eyes, conjunctivitis; very rarely - ringing in the ears, violation taste sensations. Other: infrequently - weight gain; very rarely - arthralgia, thrombocytopenia. Taking the drug Egilok ® should be discontinued if any of the above effects reaches a clinically significant intensity, and its cause cannot be reliably established.

Symptoms: pronounced decrease in blood pressure, sinus bradycardia, atrioventricular block, heart failure, cardiogenic shock, asystole, nausea, vomiting, bronchospasm, cyanosis, hypoglycemia, loss of consciousness, coma. The symptoms listed above may increase with the simultaneous use of ethanol, antihypertensive drugs, quinidine and barbiturates.
The first symptoms of an overdose appear 20 minutes -2 hours after taking the drug.

Treatment: it is necessary to carefully monitor the patient (control of blood pressure, heart rate, respiratory rate, kidney function, blood glucose concentration, blood serum electrolytes) in the conditions of the department intensive care. If the drug has been taken recently, gastric lavage with activated charcoal may reduce further absorption of the drug (if lavage is not possible, vomiting can be induced if the patient is conscious).

In case of an excessive decrease in blood pressure, bradycardia and the threat of heart failure - in / in, with an interval of 2-5 minutes, beta-agonists - until the desired effect is achieved or in / in 0.5-2 mg of atropine. With absence positive effect- dopamine, dobutamine or norepinephrine (norepinephrine). With hypoglycemia - the introduction of 1-10 mg of glucagon, the installation of a temporary pacemaker. With bronchospasm, beta2-agonists should be administered. With convulsions - slow intravenous administration of diazepam. Hemodialysis is ineffective.

INTERACTIONS WITH OTHER DRUGS

The antihypertensive effects of the drug Egilok ® and other antihypertensive drugs are usually enhanced. In order to avoid arterial hypotension, careful monitoring of patients receiving combinations of such agents is necessary. However, the summation of the effects of antihypertensive drugs can be used if necessary to achieve effective control blood pressure.

The simultaneous use of metoprolol and blockers of "slow" calcium channels such as diltiazem and verapamil can lead to an increase in negative inotropic and chronotropic effects. The intravenous administration of calcium channel blockers such as verapamil should be avoided in patients receiving beta-blockers.

Caution should be exercised when taken concomitantly with the following agents:

Oral antiarrhythmic drugs (such as quinidine and amiodarone) - the risk of bradycardia, atrioventricular block.

Cardiac glycosides (risk of bradycardia, conduction disturbances; metoprolol does not affect the positive inotropic effect of cardiac glycosides).

Other antihypertensive drugs(especially the guanethidine, reserpine, alpha-methyldopa, clonidine and guanfacine groups) due to the risk of hypotension and/or bradycardia.

Termination simultaneous reception metoprolol and clonidine should always be started, canceling metoprolol, and then (after a few days) clonidine; if clonidine is discontinued first, a hypertensive crisis may develop.

Some drugs that act on the central nervous system, for example: sleeping pills, tranquilizers, tri- and tetracyclic antidepressants, antipsychotics and ethanol increase the risk of arterial hypotension. Means for anesthesia (risk of oppression of cardiac activity).

Alpha- and beta-sympathomimetics (risk of arterial hypertension, significant bradycardia; possibility of cardiac arrest). Ergotamine (increased vasoconstrictor effect). Beta-2 sympathomimetics (functional antagonism).

Non-steroidal anti-inflammatory drugs (eg, indomethacin) - may weaken the antihypertensive effect.

Estrogens (may reduce the antihypertensive effect of metoprolol). Oral hypoglycemic agents and insulin (metoprolol may enhance their hypoglycemic effects and mask the symptoms of hypoglycemia). Curare-like muscle relaxants (increased neuromuscular blockade). Enzyme inhibitors (for example, cimetidine, ethanol, hydralazine; selective serotonin reuptake inhibitors, for example, paroxetine, fluoxetine and sertraline) - an increase in the effects of metoprolol due to an increase in its concentration in blood plasma. Enzyme inducers (rifampicin and barbiturates): the effects of metoprolol may be reduced due to an increase in hepatic metabolism.

Simultaneous use of drugs that block the sympathetic ganglia, or other beta-blockers (for example: eye drops) or monoamine oxidase inhibitors requires careful medical supervision.

Monitoring of patients taking beta-blockers includes regular measurement of heart rate (HR) and blood pressure, blood glucose concentration in patients with diabetes mellitus. If necessary, for patients with diabetes mellitus, the dose of insulin or hypoglycemic agents for oral administration should be selected individually. The patient should be taught how to calculate heart rate and instruct about the need for medical advice if the heart rate is less than 50 beats / min. When taking a dose above 200 mg per day, cardioselectivity decreases.

In heart failure, treatment with Egilok ® is started only after reaching the stage of compensation of cardiac function.

Possible increased severity of reactions hypersensitivity and the lack of effect from the introduction of conventional doses of epinephrine (adrenaline) in patients with a aggravated allergic history.

Anaphylactic shock may be more severe in patients taking Egilok ® . May exacerbate symptoms of peripheral arterial circulatory disorders. Avoid abrupt discontinuation of the drug Egilok ® . The drug should be discontinued gradually by reducing the dose over a period of approximately 14 days. Abrupt withdrawal may exacerbate angina symptoms and increase the risk of coronary disorders. Particular attention should be paid to patients with the disease when discontinuing the drug. coronary arteries. In case of exertional angina, the selected dose of Egilok ® should provide heart rate at rest within 55-60 beats / min, with exercise - no more than 110 beats / min. Patients using contact lenses should take into account that against the background of treatment with beta-blockers, a decrease in the production of lacrimal fluid is possible. Egilok may mask some of the clinical manifestations of hyperthyroidism (eg, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, as it can exacerbate symptoms.

In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentration to normal levels. In the case of prescribing the drug Egilok ®, patients with diabetes mellitus should monitor the concentration of blood glucose and, if necessary, adjust the dose of insulin or hypoglycemic agents for oral administration (see section "Interaction with other drugs").

If it is necessary to prescribe to patients with bronchial asthma, beta2-agonists are prescribed as concomitant therapy; with pheochromocytoma - alpha-blockers.

If it is necessary to perform a surgical intervention, it is necessary to warn the surgeon / anesthetist about the therapy being carried out (the choice of a general anesthesia agent with a minimal negative inotropic effect), discontinuation of the drug is not recommended. Drugs that reduce catecholamine stores (for example, reserpine) can increase the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect excessive lowering of blood pressure or bradycardia.

In elderly patients, regular monitoring of liver function is recommended. Correction of the dosing regimen is required only if an elderly patient develops increasing bradycardia (less than 50 beats / min), a pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg), atrioventricular blockade, bronchospasm, ventricular arrhythmias, severe liver dysfunction sometimes it is necessary to stop treatment. Patients with severe kidney failure it is recommended to monitor kidney function.

Should be carried out special control for the condition of patients with depressive disorders taking metoprolol; in case of development of depression caused by taking beta-blockers, it is recommended to stop therapy.

If progressive bradycardia occurs, the dose should be reduced or the drug should be discontinued.

Due to the lack of sufficient clinical data, the drug is not recommended for use in children.

Influence on the ability to drive vehicles and complex machinery.

Care must be taken when driving vehicles and when engaging in potentially hazardous activities that require increased concentration (risk of dizziness and increased fatigue).

Tablets 25 mg: 60 tablets in a brown glass bottle with a PE cap with an accordion shock absorber, with a first opening control. 1 bottle, together with instructions for use, is packed in a cardboard box. Or 20 tablets in a PVC/PVDC//al. foil. 3 blisters, together with instructions for use, are packed in a cardboard box.